產品描述: | BMS-191095 is a selective activator of mitochondrial ATP-sensitive potassium (mitoKATP) channels. BMS-191095 inhibits human platelet aggregation by opening mitochondrial K(ATP) channels |
靶點: |
BMS-191095 (50 μmol/L) 誘導 SD 大鼠血管平滑肌細胞 (VSM) 線粒體去極化。BMS-191095 (10-100 μmol/L) 劑量依賴性地誘導內皮剝脫腦動脈血管舒張。BMS-191095 (50 μmol/L) 增加了細胞鈣火花的頻率。BMS-191095 (0-1500 μM) 抑制膠原蛋白和凝血酶誘導的人血小板聚集,IC50 分別為 63.9 和 104.8 μM;PotassiumChannel |
體外研究: |
BMS-191095 (2.5 或 25 μg;腦室內灌注,缺血誘導前 30 分鐘/60 分鐘/24 小時,1次) 可減輕短暫性局灶性腦缺血對大鼠神經元的損傷。 Animal Model: Male Wistar rats with the induction of ischemia induced by middle cerebral artery occlusion (MCAO) Dosage: 2.5 or 25 μg Administration: Intraventricular infusion; 30 min/60 min/24 hours before the induction of ischemia, once Result: Reduced total infarct volume in rats with of pretreat dose of 25 mg and 24 h before MCA. Induced a rapid mitochondrial depolarization. |
參考文獻: |
1. Katakam PV, et al. Diversity of mitochondria-dependent dilator mechanisms in vascular smooth muscle of cerebral arteries from normal and insulin-resistant rats. Am J Physiol Heart Circ Physiol. 2014 Aug 15;307(4):H493-503. 2. Cho MR, et al. BMS-191095, a cardioselective mitochondrial K(ATP) opener, inhibits human platelet aggregation by opening mitochondrial K(ATP) channels. Arch Pharm Res. 2005 Jan;28(1):61-7. 3. Mayanagi K, et al. The mitochondrial K(ATP) channel opener BMS-191095 reduces neuronal damage after transient focal cerebral ischemia in rats. J Cereb Blood Flow Metab. 2007 Feb;27(2):348-55. |
溶解性: |
soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.446 ml |
12.229 ml |
24.457 ml |
5 mM |
0.489 ml |
2.446 ml |
4.891 ml |
10 mM |
0.245 ml |
1.223 ml |
2.446 ml |
50 mM |
0.049 ml |
0.245 ml |
0.489 ml |
|
注意: |
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